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1.
M. E. Kon’shin A. L. Efremov M. I. Vakhrin A. A. Gorbunov 《Russian Journal of Organic Chemistry》2012,48(4):544-546
Reactions of 2-(phenylamino)benzoic and 2-(phenylamino)- and 2-methyl-6-phenylpyridine-3-carboxylic acid hydrazides with succinic
anhydride in organic solvents at room temperature gave the corresponding 4-(2-aroylhydrazinyl)-4-oxobutanoic acids. The reactions
in boiling acetic acid afforded N-(2,5-dioxopyrrolidin-1-yl)benzamide or N-(2,5-dioxopyrrolidin-1-yl)pyridine-3-carboxamide. 相似文献
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A series of condensation products of 1-(9-butylcarbazol-3-yl)-5-oxopyrrolidine-3-carbohydrazide with 2-propanone, 2-butanone,
2,4-pentanedione, 2,5-hexanedione, ethyl 3-oxobutanoate, and aromatic aldehydes was obtained. Substituted oxadiazoles were
synthesized from carbohydrazide or the corresponding hydrazone. Spectral properties of the synthesized compounds were examined.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 1009–1017, July, 2008. 相似文献
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Marc Lang Ernst Hungerbühler Peter Schneider Riccardo Scartazzini Werner Tosch Edward A. Konopka Oto Zak 《Helvetica chimica acta》1986,69(7):1576-1580
In continuation of our work on penem antibiotics, novel chiral (5R,6S)-2-(1′-aminoalkyl)-6-(hydroxyalkyl)-derivatives 1 have been synthesized by two essentially different strategies. Whereas the starting materials for 1a - f , azetidinones 2 and 5 , were obtained from chiral building blocks (6-aminopenicillanic acid and L-threonine, resp.), the one for 1g , azetidinone 9 , was derived from racemic 4-acetoxyazetidinone and, as chiral auxiliary, (2R)-2-mercaptopropan-1-ol. The 2-aminomethyl derivatives 1a (CGP 30 779) and 1f (CGP 31 608) proved the most potent compounds in the antibacterial tests in vitro and showed a well-balanced spectrum of activity by comparison with that of established β-lactams. 相似文献
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Bernard Aebischer Peter Frey Hans-Peter Haerter Paul L. Herrling Werner Mueller Henry J. Olverman Jeffrey C. Watkins 《Helvetica chimica acta》1989,72(5):1043-1051
The (R)- and (s)-enantiomers of 4-(3-phosphonopropyl)piperazine-2-carboxylic acid (D - and L -CPP, resp.; 15 and 16 , resp.), and of its unsaturated analogue (E)-4-(3-phosphonoprop-2-enyl)piperazine-2-carboxylic acid (D - and L -CPP-ene, resp.; 13 and 14 , resp.) were prepared. The absolute configuration of the enantiomers was determined by a chemical correlation of the menthyl ester 7 with D -asparagine. The affinity of these derivatives for the NMDA receptor was determined by displacement of [3H]CPP in rat cerebral cortical membranes. In two functional tests (the frog hemisected spinal cord preparation and the sodium efflux test from rat brain slices), D -CPP-ene appears to be the most potent, enantiomerically pure, competitive NMDA antagonist known to date. 相似文献
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A synthetic scheme extensively utilizing silylation-desilylation reactions to achieve the total synthesis of 2,6-substituted carbapenem antibiotics from readily available azetidinones is reported. An epimeric pair of new 2,6-substituted carbapenems, (±)-2-cyclopropyl-6-(1′-hydroxyethyl)-1-carbapen-2-em-3-carboxylic acids were synthesized. 相似文献
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As a part of metabolic studies of mosapride ( 1 ), a potential gastroprokinetic agent, the synthesis of 4-chloro-7-ethoxy-2(3H)-benzoxazolone-6-carboxylic acid ( 7 ) as a derivative of 4-amino-5-chloro-2-ethoxy-3-hydroxybenzoic acid ( 6 ), which has served a benzoic acid part of the metabolites 4 and 5 , is described. Treatment of methyl 3-amino-4-substituted amino-5-chloro-2-ethoxybenzoate derivatives 11a-c with sodium nitrate in acidic medium gave the benzotriazole derivatives 13x,y instead of the objective 3-hydroxy counterpart. The synthesis of 7 started from o-vanillin acetate ( 15 ) and proceeded through the intermediates 2-hydroxy-3-methoxy-4-nitrobenzaldehyde ( 18 ), methyl 4-amino-2,3-dihydroxybenzoate ( 23 ), and methyl 7-hydroxy-2(3H)-benzoxazolone-6-carboxylate ( 30 ). Compound 30 was alternatively prepared from 23 via methyl 4-ethoxycarbonylamino-2-ethoxycarbonyloxy-3-hydroxybenzoate ( 29 ), which is the product resulting from the migration of the ethoxycarbonyl group of methyl 4-amino-2,3-diethoxycar-bonyloxybenzoate ( 27 ). 相似文献
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《Tetrahedron: Asymmetry》2007,18(18):2125-2128
Lipase-catalyzed esterification of (±)-methyl 1′-(1-hydroxyethyl)ferrocene-1-carboxylate 4 afforded its (R)-acetate (−)-5 (ee = 99%) and (S)-(+)-4 (ee = 90%). Stereoretentive azidation/amination/acetylation of (R)-(−)-5 gave (R)-(+)-methyl 1′-(1-acetamidoethyl)ferrocene-1-carboxylate (R)-3 (ee = 98%). In a similar manner (S)-(+)-4 was converted into (S)-(−)-3 (ee = 84%). Both enantiomers of 3 were obtained in high chemical yields without a loss of enantiomeric purity. The title compounds can be coupled with natural amino acids and peptides on both C- and N-termini. 相似文献
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A. Yu. Ershov D. G. Nasledov E. V. Parilova I. V. Lagoda V. V. Shamanin 《Russian Journal of Organic Chemistry》2014,50(8):1164-1174
Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohydropyrimidine-4-carboxylic acids, potential antihypertensive drugs, inhibitors of the angiotensin converting enzyme. 相似文献
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Jordi Bols Santiago Gubert Lluís Anglada Angel Prez Aurelio Sacristn Jos A. Ortiz 《Journal of heterocyclic chemistry》1994,31(6):1493-1496
The synthesis of the novel amino acid 6-(hydroxymethyl)-2-piperidinecarboxylic acid ( 1a ) and its ethyl ester 1b is reported. In the hydrogenation of 6-(hydroxymethyl)pyridine-2-carboxylates, hydrogenolysis of the alcohol group appeared as an unusual side reaction. Optimization of the reaction conditions allowed us to minimize hydrogenolysis and afforded pure 1 . 相似文献
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Gorodnicheva N. V. Vasil´eva O. S. Ostroglyadov E. S. Baichurin R. I. Makarenko S. V. Karamov F. A. Lodochnikova O. A. Litvinov I. A. 《Russian Chemical Bulletin》2020,69(3):470-486
Russian Chemical Bulletin - 4-Het(aryl)-2-pyrrolidone-3(5)-carboxylic acid hydrazides react with aromatic aldehydes, acetone, and acetophenone to give new representatives of... 相似文献
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S Kishimoto T Aono Y Araki I Minamida K Tanaka 《Chemical & pharmaceutical bulletin》1974,22(10):2231-2241
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Crystal structure and photoluminescence of 7-(N,N'-diethylamino)-coumarin-3-carboxylic acid 总被引:1,自引:0,他引:1
Zhang H Yu T Zhao Y Fan D Chen L Qiu Y Qian L Zhang K Yang C 《Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy》2008,69(4):1136-1139
The structure of 7-(N,N'-diethylamino)-coumarin-3-carboxylic acid (DCCA) was verified by single crystal X-ray crystallography. The UV-vis absorption and fluorescence of DCCA were discussed. The compound exhibits strong blue emission under ultraviolet light excitation. The molecular structure of DCCA was optimized using density function theory (DFT) at B3LYP/6-31G level, showing that the optimized geometers parameters are in good agreement with experiment data. In addition, the HOMO and LUMO levels of DCCA were deduced. 相似文献
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The annulation of the oxyacetic chain of thienylic acid into a γ-pyrone ring is described. The resulting 6-(2-thenoyl)-7,8-dichloro-4-oxo-4H-1-benzopyran-2-carboxylic acid retains almost 80% of the diuretic activity of the parent compound. 相似文献
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Nathan J. Line 《Tetrahedron letters》2019,60(20):1357-1358
A practical enantioselective synthesis of (3S, 4R)-3-hydroxypiperidine-4-carboxylic acid was accomplished via an unconventional Evans anti-aldol reaction followed by a one-pot azide reduction/reductive cyclization. 相似文献